ChemicalBook > CAS DataBase List > CB5083
CB5083
- Product Name
- CB5083
- CAS No.
- 1542705-92-9
- Chemical Name
- CB5083
- Synonyms
- CB5083;CS-1553;CB-5083;EOS-61078;CB 5083;CB5083;CB5083; CB-5083; CB 5083.;1-[4-(benzylamino)-5H,7H,8H-pyrano[4,3-d]pyrimidin-2-yl]-2-methyl-1H-indole-4-carboxamide;1-[4-(benzylamino)-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-2-yl]-2-methylindole-4-carboxamide;1-(4-(benzylamino)-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-2-yl)-2-methyl-1H-indole-4-carboxamide;1H-Indole-4-carboxamide, 1-[7,8-dihydro-4-[(phenylmethyl)amino]-5H-pyrano[4,3-d]pyrimidin-2-yl]-2-methyl-
- CBNumber
- CB72749007
- Molecular Formula
- C24H23N5O2
- Formula Weight
- 413.47
- MOL File
- 1542705-92-9.mol
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CB5083 Property
- Boiling point:
- 760.5±70.0 °C(Predicted)
- Density
- 1.37±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- insoluble in H2O; ≥20.65 mg/mL in DMSO; ≥4.4 mg/mL in EtOH
- form
- solid
- pka
- 15.99±0.30(Predicted)
- color
- White to light yellow
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N-Bromosuccinimide Price
Cayman Chemical
- Product number
- 19311
- Product name
- CB-5083
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
Cayman Chemical
- Product number
- 19311
- Product name
- CB-5083
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $132
- Updated
- 2024/03/01
Cayman Chemical
- Product number
- 19311
- Product name
- CB-5083
- Purity
- ≥95%
- Packaging
- 10mg
- Price
- $242
- Updated
- 2024/03/01
Cayman Chemical
- Product number
- 19311
- Product name
- CB-5083
- Purity
- ≥95%
- Packaging
- 25mg
- Price
- $548
- Updated
- 2024/03/01
ChemScene
- Product number
- CS-5405
- Product name
- CB-5083
- Purity
- 99.95%
- Packaging
- 5mg
- Price
- $50
- Updated
- 2021/12/16
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CB5083 Chemical Properties,Usage,Production
Biological Activity
cb-5083 is an orally bioavailable inhibitor of p97. p97 is an aaa-atpase involved in multiple cellular functions such as organelle membrane homotypic fusion and sorting of endosomal cargo. p97 is also known as valosin-containing protein which plays important roles in regulating protein homeostasis [1].
in vitro
cb-5083 is a selective potent inhibitor of p97’s second atpase domain. cb-5083 might compete with atp for the same binding site but may adopt a different orientation[2]. the ic50 of cb-5083 against wild-type (wt) p97 was 15.4 nm. cb-5083 could dose-dependently increase the cytosolic protein degradation in hek293t, a549 and hct116 cell lines [1]. cb-5083 treatment (2.5 μm) of a549 cells for 24h could induce cancer cell death [1].
in vivo
in female nude mice bearing hct116, a549 lung carcinoma, and amo-1 multiple myeloma xenograft tumors, oral administration of cb-5083 (100 mg/kg) for 6 h showed a significant antitumor response in tumors (tgi = 63%, p < 0.0001) [1,2].
IC 50
15.4 nm
storage
Store at -20°C
References
anderson d j, le moigne r, djakovic s, et al. targeting the aaa atpase p97 as an approach to treat cancer through disruption of protein homeostasis[j]. cancer cell, 2015, 28(5): 653-665.zhou h j, wang j, yao b, et al. discovery of a first-in-class, potent, selective, and orally bioavailable inhibitor of the p97 aaa atpase (cb-5083)[j]. journal of medicinal chemistry, 2015, 58(24): 9480-9497.
CB5083 Preparation Products And Raw materials
Raw materials
Preparation Products
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